Synthesis of Clinical-Grade [(18)F]-Fluoroestradiol as a Surrogate PET Biomarker for the Evaluation of Estrogen Receptor-Targeting Therapeutic Drug.

International journal of molecular imaging Pub Date : 2013-01-01 Epub Date: 2013-05-09 DOI:10.1155/2013/278607

Manish Dixit, Jianfeng Shi, Ling Wei, George Afari, Sibaprasad Bhattacharyya

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Abstract

16 α -[(18)F]-fluoroestradiol ([(18)F]FES), a steroid-based positron emission tomography (PET) tracer, has emerged as a dependable tracer for the evaluation and management of estrogen receptor-positive (ER+) breast cancer patients. We have developed a fully automatic, one-pot procedure for the synthesis of [(18)F]FES using the Eckert & Ziegler (E & Z) radiomodular system. After [(18)F]fluorination, the intermediate was hydrolyzed with 2.0 M HCl twice and neutralized with sodium bicarbonate. After high-performance liquid chromatography (HPLC) purification, the decay-corrected radiochemical yield and purity of [(18)F]FES were 40 ± 5.0% (n = 12) and >97%, respectively. The product was stable up to 10 h. Total synthesis time including HPLC purification was 80 min. This new, fully automated rapid synthetic procedure provided high and reproducible yields of [(18)F]FES. Quality control (QC) tests showed that the [(18)F]FES produced by this method met all specifications for human injection.

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合成临床级[(18)F]-氟雌二醇，作为评估雌激素受体靶向治疗药物的替代 PET 生物标记物。

16 α-[(18)F]-氟雌二醇（[(18)F]FES）是一种基于类固醇的正电子发射断层扫描（PET）示踪剂，已成为评估和治疗雌激素受体阳性（ER+）乳腺癌患者的可靠示踪剂。我们利用 Eckert & Ziegler (E & Z) 放射调制系统开发了一种全自动的单锅程序，用于合成[(18)F]FES。[(18)F]氟化后，中间体用 2.0 M HCl 水解两次，并用碳酸氢钠中和。经高效液相色谱（HPLC）纯化后，[(18)F]FES 的衰变校正放射化学收率和纯度分别为 40 ± 5.0% (n = 12) 和 >97%。包括 HPLC 纯化在内的总合成时间为 80 分钟。这种全新的全自动快速合成程序可提供高产率和可重复性的[(18)F]FES。质量控制（QC）测试表明，该方法制备的[(18)F]FES 符合人体注射用的所有规格。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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International journal of molecular imaging

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